(-)-Huperzine A (HupA)

製品コードS2251 バッチS225101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H18N2O
分子量 242.32 CAS No. 102518-79-6
Solubility (25°C)* 体外 5%TFA 7.54 mg/mL (31.11 mM)
DMSO Insoluble
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 (-)-Huperzine A is a potent, highly specific and reversible inhibitor of acetylcholinesterase (AChE) with Ki of 7 nM, exhibiting 200-fold more selectivity for G4 AChE over G1 AChE. Also acts as an NMDA receptor antagonist. Phase 4.
in vitro (-)-Huperzine A is a novel alkaloid isolated from the Chinese herb Huperzia serrata. (-)-Huperzine A preferentially inhibits tetrameric AChE (G4 form). (-)-Huperzine A is more potent than tacrine, physostigmine, galanthamine, and rivastigmine with respect to inhibition of AChE activity, whereas HupA is the least potent BuChE inhibitor among the inhibitors. [1] (-)-Huperzine A possesses the ability to protect cells against hydrogen peroxide, β-amyloid protein, glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress, regulate the expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism. [3]
in vivo (-)-Huperzine A can ameliorate the learning and memory deficiency in animal models and AD patients. Its potentially beneficial actions include modification of β-amyloid peptide processing, reduction of oxidative stress, neuronal protection against apoptosis, and regulation of the expression and secretion of nerve growth factor (NGF) and NGF signaling. [2] (-)-Huperzine A significantly inhibits AChE activity in the cortex, hippocampus, striatum, medial septum, medulla oblongata, cerebellum, and hypothalamus of rats that are killed 30 min following the administration of (-)-Huperzine A at several dose levels compared with the saline control. [3]
特徴 Greater penetration of the blood-brain barrier, higher oral bioavailability, and longer AChE inhibition relative to tacrine, donepezil, and rivastigmine.

プロトコル(参考用のみ)

キナーゼアッセイ In vitro assay of brain acetylcholinesterase
Adult Sprague-Dawley male rats are decapitated, the brain is rapidly dissected on ice into cortex, hippocampus and striatum, and then weighed and homogenized in five volumes of cold 75 mM sodium phosphate buffer, pH 7.4. Homogenates are centrifuged at 13 000 g for 30 min at 4 °C; supernatants used as acetylcholinesterase sources are divided into aliquots and stored at −20 °C. Acetylcholinesterase activity is measured by the principle of the Ellman method. Enzyme samples in 10 mM phosphate buffer, pH 7.5, are incubated 150 s at 37 °C with 0.3 mM acetylthiocholine iodide in the presence of 50 μM tetraisopropyl pyrophosphoramide, a selective inhibitor of butyrylcholinesterase, and 5,5′-dithiobis-(2-nitrobenzoic acid), for color development. Production of the yellow anion of 5-thio-2-nitro-benzoic acid is measured with a SPECTRAmax 96-well plate reader at 412 nm. Protein concentration is measured with the Coomassie brilliant blue protein-binding method using bovine serum albumin as standard. Acetylcholinesterase activity is expressed in international units (1 IU=1 μmol acetylthiocholine hydrolyzed per second) per mg protein.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 0.1 mg/kg
投与方法 Orally

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Donepezil, a drug for Alzheimer's disease, promotes oligodendrocyte generation and remyelination. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-018-0206-4] PubMed: 30918344

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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